Structure-Activity Relationships of the Dimeric Analogues of Endomorphin-2 with Different Lengths of Spacers

Title: Structure-Activity Relationships of the Dimeric Analogues of Endomorphin-2 with Different Lengths of Spacers

Volume: 15 Issue: 3

Author(s): Yuan-Ming Qi, Yan-Feng Gao, Ming-Xia Zhai, Wei-Xia Liu, Xin Liu, Ye Yuan and Rui Wang

Affiliation:

Keywords: Endomorphin-2, Dimerization, analogue, Structure-activity relationships, Opioid receptor, balanced agonist

Abstract: In the present study, seven novel dimeric analogues of endomorphin-2 with longer spacers were designed and synthesized. Through dimerization, their affinity for δ-opioid receptor was mostly increased, especially the δ-opioid receptor preferred dimeric analogue, DEM12. The results were confirmed by the in vitro bioassay. The structure-activity relationships were also discussed.

Cite this article as:

Qi Yuan-Ming, Gao Yan-Feng, Zhai Ming-Xia, Liu Wei-Xia, Liu Xin, Yuan Ye and Wang Rui, Structure-Activity Relationships of the Dimeric Analogues of Endomorphin-2 with Different Lengths of Spacers, Protein & Peptide Letters 2008; 15 (3) . https://dx.doi.org/10.2174/092986608783744199